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1. 发明专利

JP2006104214A Kappa receptor selective opioid peptides 审中-公开
标题翻译： KAPPA受体选择性OPIOID PEPTIDES
公开(公告)号：JP2006104214A
公开(公告)日：2006-04-20
申请号：JP2005365634
申请日：2005-12-19
申请人： Torrey Pines Inst For Molecular Studies , トーレイパインズインスティテュートフォーモレキュラースタディーズ
发明人： DOOLEY COLETTE T , HOUGHTEN RICHARD A
IPC分类号： A61K38/00 , C07K5/107 , A61K31/00 , A61K38/22 , A61P25/00 , A61P25/02 , A61P25/04 , C07K5/103 , C07K7/06 , C07K14/665
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K5/1016 , C07K14/665
摘要： PROBLEM TO BE SOLVED: To provide a plurality of individual peptides in order to use in the biomedical research including the research for studying the mutual action between opiate ligand and receptor.
SOLUTION: A peptide having the following structure: Ac-A1-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (SEQ ID NO. 28) wherein A1 is Tyr or Arg, B2 is Arg or Phe and C3 is Tyr, Phe or Met, for example, having the sequences selected from the following group: the specific peptides:Ac-Tyr-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (SEQ ID NO. 1); Ac-Tyr-Arg-Phe-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (SEQ ID NO. 2);Ac-Arg-Phe-Phe-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (SEQ ID NO. 3);Ac-Tyr-Arg-Met-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (SEQ ID NO. 4) andAc-Arg-Arg-Phe-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (SEQ ID NO. 5).
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：为了在生物医学研究中使用多个单独的肽，包括研究阿片剂配体和受体之间的相互作用的研究。解决方案：具有以下结构的肽：Ac-A1-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH 2（SEQ ID NO.28）其中A1是Tyr或Arg，B2是Arg或Phe，C3是Tyr，Phe或Met，例如具有选自以下组的序列：特异性肽：Ac-Tyr-Arg-Tyr-Arg-Tyr-Arg -Arg-Arg-NH 2（SEQ ID NO.1）; Ac-Tyr-Arg-Phe-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH 2（SEQ ID NO.2）; Ac-Arg-Phe-Phe-Arg-Tyr -Arg-Tyr-Arg-Arg-Arg-NH 2（SEQ ID NO.3）; Ac-Tyr-Arg-Met-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg- （SEQ ID NO.4）和Ac-Arg-Arg-Phe-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NHS2（SEQ ID NO：第5号）。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JP2007077163A New kappa receptor-selective opioid peptide 有权
标题翻译：新型KAPPA受体选择性OPIOID PEPTIDE
公开(公告)号：JP2007077163A
公开(公告)日：2007-03-29
申请号：JP2006297157
申请日：2006-10-31
申请人： Torrey Pines Inst For Molecular Studies , トーレイパインズインスティテュートフォーモレキュラースタディーズ
发明人： DOOLEY COLETTE T , HOUGHTEN RICHARD A
IPC分类号： A61K38/00 , C07K7/06 , A61K31/00 , A61P25/00 , A61P25/02 , C07K5/10 , C07K5/103 , C07K5/107 , C07K14/665
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K5/1016 , C07K14/665
摘要： PROBLEM TO BE SOLVED: To provide many individual peptides for use in a biomedicinal investigation including the investigation for study of opiate ligand-receptor interaction.
SOLUTION: The peptide has the structure of Ac-A1-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH
2 (wherein A1 is Tyr or Arg; B2 is Arg or Phe; and C3 is Thr, Phe, or Met).
COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供用于生物医学研究的许多单独的肽，包括研究阿片剂配体 - 受体相互作用的研究。解决方案：该肽具有Ac-A1-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH 2 的结构（其中A1是Tyr或Arg; B2是Arg或Phe;和C3是Thr，Phe或Met）。版权所有（C）2007，JPO＆INPIT

3. 发明公开

EP0853484A4 NOVEL MU OPIOID RECEPTOR LIGANDS: AGONISTS AND ANTAGONISTS 失效
标题翻译： MU-OPIOIDLIGANDE：AGONISTEN UND ANTAGONISTEN
公开(公告)号：EP0853484A4
公开(公告)日：1999-11-03
申请号：EP96919169
申请日：1996-06-06
申请人： TORREY PINES INST
发明人： DOOLEY COLETTE T , HOUGHTEN RICHARD A
IPC分类号： A61K38/00 , C07K5/087 , C07K5/107 , C07K5/117 , C07K7/06 , C07K14/665 , A61K38/08
CPC分类号： C07K7/06 , A61K38/00 , C07K5/0812 , C07K5/1016 , C07K5/1024 , C07K14/665
摘要： The present invention provides novel opioid peptides. Disclosed are opioid peptides having the general structure Ac-Phe-Arg-Trp-Trp-Tyr-Xaa-NH2 (SEQ ID No. 1); Ac-Arg-Trp-Ile-Gly-Trp-Xaa-NH2 (SEQ ID No. 2); Trp-Trp-Pro-Lys/Arg-Hisz-Xaaz-NH2 (SEQ ID No. 222); Tyr-Pro-Phe-Gly-Phe-Xaa-NH2 (SEQ ID No. 5); (D)Ile-(D)Met-(D)Ser-(D)Trp-(D)Trp-Glyn-Xaa-NH2 (SEQ ID No. 6); and (D)Ile-(D)Met-(D)Thr-(D)Trp-Gly-Xaa-NH2 (SEQ ID No. 7). Within each genus, Xaa is substituted by a specific amino acid. The invention also relates to an opioid peptide having general structure Tyr-A1-B2-C3-NH2 (SEQ ID No. 8), wherein A is D-Nve or D-Nle, B is Gly, Phe, or Trp, and C is Trp or Nap. Also included within the invention are opioid compounds of the general structure MexHyN-Tyr-Tyr-Phez-Proz-NH2 (SEQ ID No. 221) which are peptides modified by permethylation, perallylation, perethylation, perbenzylation or pernaphthylation and which be further modified by reduction.
摘要翻译：本发明提供新的阿片样肽。公开了具有通式结构Ac-Phe-Arg-Trp-Trp-Tyr-Xaa-NH 2（SEQ ID No.1）的阿片样肽; Ac-Arg-Trp-Ile-Gly-Trp-Xaa-NH 2（SEQ ID No.2）; Trp-Trp-Pro-Lys / Arg-Hisz-Xaaz-NH2（SEQ ID No.222）; Tyr-Pro-Phe-Gly-Phe-Xaa-NH2（SEQ ID No.5）; （D）Ile-（D）Met-（D）Ser-（D）Trp-（D）Trp-Glyn-Xaa-NH2（SEQ ID No.6）; 和（D）Ile-（D）Met-（D）Thr-（D）Trp-Gly-Xaa-NH 2（SEQ ID No.7）。在每个属中，Xaa被特定氨基酸取代。本发明还涉及具有一般结构Tyr-A1-B2-C3-NH2（SEQ ID No.8）的阿片样肽，其中A是D-Nve或D-Nle，B是Gly，Phe或Trp，C 是Trp或Nap。本发明还包括通用结构MexHyN-Tyr-Tyr-Phez-Proz-NH2（SEQ ID No.222）的阿片样化合物，它们是通过甲基化，过氧化，乙酰化，过苯甲酰化或全萘基化修饰的肽，并进一步被减少。

4. 发明申请

WO2007047551A3 METHODS AND COMPOSITIONS FOR DEREPRESSION OF IAP-INHIBITED CASPASE 审中-公开
标题翻译：用于抑制IAP抑制性CASPASE的方法和组合物
公开(公告)号：WO2007047551A3
公开(公告)日：2007-06-21
申请号：PCT/US2006040301
申请日：2006-10-13
申请人： BURNHAM INST , TORREY PINES INST , REED JOHN C , HOUGHTEN RICHARD A , NEFZI ADEL , OSTRESH JOHN M , PINILLA CLEMENCIA , WELSH KATE
发明人： REED JOHN C , HOUGHTEN RICHARD A , NEFZI ADEL , OSTRESH JOHN M , PINILLA CLEMENCIA , WELSH KATE
IPC分类号： A61K38/00
CPC分类号： A61K31/337 , A61K31/17 , A61K31/704 , A61K31/7048 , A61K38/1761 , A61K45/06 , G01N33/573 , G01N2333/95 , G01N2500/02 , G01N2510/00 , A61K2300/00
摘要： The invention provides isolated agents having a core peptide selected from the group consisting of Core peptides 5 through 39 and 42 through 55, wherein the agent derepresses an IAP-inhibited caspase. Also provided is an isolated agent having a core structure selected from any of the structures shown in Figures 5, 9, 10, 14B, 21-24 and 48, a core structure selected from the group of TPI 759, TPI 882, TPI 914 or TPI 927; and a core structure from a library selected from TPI 1391, TPI 1349, TPI 1396, TPI 1509, TPI 1540, TPI 1400, TPI 792, TPI 1332, TPI 1567, TPI 1576 and TPI 1577, wherein the agent derepresses an IAPinhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase.
摘要翻译：本发明提供了具有选自核心肽5至39和42至55的核心肽的分离的试剂，其中所述试剂减阻IAP抑制的半胱天冬酶。还提供了具有选自图5，图9，图10，图14B，图21-24和48中所示的任何结构的核心结构的分离剂，选自TPI 759，TPI 882，TPI 914或 TPI 927; 和选自TPI1391，TPI1349，TPI1396，TPI1509，TPI1540，TPI1400，TPI792，TPI1332，TPI1567，TPI1576和TPI1577的库的核心结构，其中所述试剂去抑制IAP抑制的半胱天冬酶。本发明还提供了一种抑制IAP抑制的半胱天冬酶的方法。

5. 发明公开

EP1465649A4 METHODS AND COMPOSITIONS FOR DEREPRESSION OF IAP-INHIBITED CASPASE 审中-公开
标题翻译：方法和组合物去抑制IAP抑制的半胱氨酸蛋白酶
公开(公告)号：EP1465649A4
公开(公告)日：2007-07-11
申请号：EP02793997
申请日：2002-11-21
申请人： BURNHAM INST , TORREY PINES INST
发明人： REED JOHN C , HOUGHTEN RICHARD A , NEFZI ADEL , OSTRESH JOHN M , PINILLA CLEMENCIA , WELSH KATE
IPC分类号： C12Q1/02 , A61K38/00 , A61P1/04 , A61P3/10 , A61P5/16 , A61P9/10 , A61P17/06 , A61P19/02 , A61P21/00 , A61P21/04 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07K5/10 , C07K5/103 , C07K5/107 , C07K5/11 , C07K5/117 , C07K7/04 , C07K7/06 , C12Q1/37
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1008 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K5/1027
摘要： The invention provides isolated agents having a core peptide selected from the group consisting of Core peptides 5 through 39 and 42 through 55, wherein the agent derepresses an IAP-inhibited caspase. Also provided is an isolated agent having a core structure selected from any of the structures shown in Figures 5, 9, 10, 14B, and 21-24 wherein said agent derepresses an IAP-inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The method consists of contacting an IAP-inhibited caspase with an effective amount of an agent to derepress an IAP-inhibited caspase, the agent having a core motif selected from the group consisting of a core peptide having a sequence set forth in any of Core peptides 4 through 39 and 42 through 55, and a core structure selected from the group consisting of TPI759, TPI882,TPI914 or TPI927. The methods of the invention also can be used for promoting apoptosis in a cell and for reducing the severity of a pathology characterized by reduced levels of apoptosis. Methods for identifying agents that derepress an IAP-inhibited caspase are also provided.

6. 发明公开

EP1218337A4 SYNTHESIS OF 3,5,7]-1H-IMIDAZO 1,5-A]IMIDAZOL-2(3H)-ONE COMPOUNDS 有权
标题翻译：制备[3,5,7] -1H-咪唑并[1,5-a]咪唑-2（3H） - 酮化合物的
公开(公告)号：EP1218337A4
公开(公告)日：2002-09-11
申请号：EP00961864
申请日：2000-09-13
申请人： TORREY PINES INST
发明人： ELABDELLAOUI HASSAN M , OSTRESH JOHN M , HOUGHTEN RICHARD A
IPC分类号： C07B61/00 , C07D487/04 , C07C235/02 , A61K31/415
CPC分类号： C07D487/04 , C40B40/00
摘要： Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.

7. 发明公开

EP0833652A4 NOVEL KAPPA RECEPTOR SELECTIVE OPIOID PEPTIDES 失效
标题翻译：新的阿片肽，选择性KAPPA受体
公开(公告)号：EP0833652A4
公开(公告)日：2001-10-31
申请号：EP96918080
申请日：1996-06-03
申请人： TORREY PINES INST
发明人： DOOLEY COLETTE T , HOUGHTEN RICHARD A
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/02 , C07K5/103 , C07K5/107 , C07K7/06 , C07K14/665 , A61K38/07 , A61K38/08 , C07K5/10
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K5/1016 , C07K14/665
摘要： The present invention provides novel opioid peptides which are selective for the kappa opiate receptor. In one embodiment, the kappa-selective opioid peptides have the general structure Ac-A1-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH2, (SEQ ID NO. 28), wherein A1 is Tyr or Arg, B2 is Arg or Phe, and C3 is Thr, Phe, or Met. In yet other embodiments, the kappa-selective opioid peptides have the general structure (D)Phe-D4-E5-F6 (SEQ ID NO. 29) or (D)Nle-D4-E5-F6 (SEQ ID NO. 30), where in both of these formulae D4 is (D)NapAla or (D)Phe, E5 is (D)Nle, Trp, or (D)Ile, and F6 is (D)Arg or (D)ChAla.

8. 发明公开

EP1951278A4 METHODS AND COMPOSITIONS FOR DEREPRESSION OF IAP-INHIBITED CASPASE 审中-公开
标题翻译：方法和组合物去抑制IAP-抑制胱天蛋白酶
公开(公告)号：EP1951278A4
公开(公告)日：2010-07-07
申请号：EP06825997
申请日：2006-10-13
申请人： BURNHAM INST , TORREY PINES INST
发明人： REED JOHN C , HOUGHTEN RICHARD A , NEFZI ADEL , OSTRESH JOHN M , PINILLA CLEMENCIA , WELSH KATE
IPC分类号： A61K38/00 , G01N33/573
CPC分类号： A61K31/337 , A61K31/17 , A61K31/704 , A61K31/7048 , A61K38/1761 , A61K45/06 , G01N33/573 , G01N2333/95 , G01N2500/02 , G01N2510/00 , A61K2300/00

9. 发明公开

EP0890101A4 SELECTIVELY N-ALKYLATED PEPTIDOMIMETIC COMBINATORIAL LIBRARIES AND COMPOUNDS THEREIN 失效
标题翻译：选择性N-烷基化的肽模拟物，组合文库和相关链接
公开(公告)号：EP0890101A4
公开(公告)日：1999-12-08
申请号：EP97908448
申请日：1997-03-05
申请人： TORREY PINES INST
发明人： DORNER BARBARA , OSTRESH JOHN M , DOOLEY COLLETTE T , EICHLER JUTTA , HOUGHTEN RICHARD A
IPC分类号： G01N33/50 , A61K31/16 , A61K38/00 , A61P29/00 , C07B61/00 , C07C217/62 , C07C237/20 , C07K1/04 , C07K2/00 , G01N33/15 , G01N33/543 , G01N33/566 , G01N33/53
CPC分类号： C07K1/047

10. 发明公开

EP0831872A4 POLYPEPTIDE COMPOUNDS THAT FORM BETA SHEETS 失效
标题翻译：多肽化合物BETA文件夹结构来训练
公开(公告)号：EP0831872A4
公开(公告)日：2002-10-28
申请号：EP96920441
申请日：1996-05-23
申请人： TORREY PINES INST
发明人： BLONDELLE SYLVIE E , PEREZ-PAYA ENRIQUE , FOROOD BEHROUZ , HOUGHTEN RICHARD A
IPC分类号： A61K38/00 , C07K7/08 , C07K14/00 , C12N9/16 , C12N9/24 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K7/08 , A61K38/00 , C07K14/001 , C12N9/16
摘要： The present invention is directed to a polypeptide compound having the following formula: JnAm1XuAm2Jn, where A is either a D- or L-alanine amino acid and m1 or m2 are 0 to about 40 with the proviso that m1 + m2 is 10 to about 40. J is a charged amino acid and n is 1 or 2. X is any amino acid except proline and u is 0 or 1. Such polypeptides form beta sheets in an aqueous environment and can be used to hydrolyze compounds.

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